ML213-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML213Cat.No.:HY-101843CASNo.:489402-47-3分⼦式:C₁₇H₂₃NO分⼦量:257.37作⽤靶点:PotassiumChannel作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:36.67mg/mL(142.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8855mL19.4273mL38.8546mL5mM0.7771mL3.8855mL7.7709mL10mM0.3885mL1.9427mL3.8855mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.75mg/mL(10.69mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(10.69mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(10.69mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ML213⼀种具有选择性的Kv7.2和Kv7.4通道增强剂，EC50值分别为230nM和510nM。IC50&TargetEC50:230nM(Kv7.2channel),510nM(Kv7.4channel)[2][3]体外研究ML213(100nM-30µM)increasesmaximalconductancetoapeakat212%±27%ofcontrol,withanEC50of0.8±0.3µM.ML213(10µM)reducesthedeactivationratesofKv7.4currentsby4.6-foldinthevoltagerangefrom−130mVto−90mV.ML213isapotentandeffectiveactivatorofhomomericKv7.5channelsoverexpressedinA7r5cells.ML213increasesmaximalconductanceofKv7.5channelswithanEC50of0.7±0.2µM.ML213(10µM)alsoreducesdeactivationratesofKv7.5currentsby5.9-foldonaverage.ML213producessimilareffectsonheteromericKv7.4/7.5channels:204%±11%maximalincreaseinconductancewithanEC50of1.1±0.6µManda34.2±3.3mVmaximalnegativeshiftoftheactivationcurve,withanEC50of3.8±1.2µM[1].ML213causesavasorelaxationindifferentprecontractedratbloodvessels.ML213(10μM)alsohyperpolarizesmesentericarterysmoothmusclecells[2].ML213causesaconcentration-dependentshiftintheV1/2forKCNQ2activationwithanEC50340±70nMandamaximalshiftof37.4mV[3].REFERENCES[1].BrueggemannLI,etal.DifferentialactivationofvascularsmoothmuscleKv7.4,Kv7.5,andKv7.4/7.5channelsbyML213andICA-069673.MolPharmacol.2014Sep;86(3):330-41.[2].JeppsTA,etal.VasorelaxanteffectsofnovelKv7.4channelenhancersML213andNS15370.BrJPharmacol.2014Oct;171(19):4413-24.[3].YuH,etal.Discovery,Synthesis,andStructureActivityRelationshipofaSeriesofN-Aryl-bicyclo[2.2.1]heptane-2-carboxamides:CharacterizationofML213asaNovelKCNQ2andKCNQ4PotassiumChannelOpener.ACSChemNeurosci.2011Oct19;2(10):572-577McePdfHeightCaution:Producthasnotbeenfullyvalidatedform